ES2502490T3 - Aminoheteroaryl compounds as protein kinase inhibitors - Google Patents
Aminoheteroaryl compounds as protein kinase inhibitors Download PDFInfo
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- ES2502490T3 ES2502490T3 ES12163855.5T ES12163855T ES2502490T3 ES 2502490 T3 ES2502490 T3 ES 2502490T3 ES 12163855 T ES12163855 T ES 12163855T ES 2502490 T3 ES2502490 T3 ES 2502490T3
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- inhibition
- aryl
- membered
- protein kinase
- cr6r7
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- 125000005214 aminoheteroaryl group Chemical group 0.000 title 1
- 229940045988 antineoplastic drug protein kinase inhibitors Drugs 0.000 title 1
- 239000003909 protein kinase inhibitor Substances 0.000 title 1
- 125000003118 aryl group Chemical group 0.000 abstract 4
- 125000001072 heteroaryl group Chemical group 0.000 abstract 4
- 125000004400 (C1-C12) alkyl group Chemical group 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000006652 (C3-C12) cycloalkyl group Chemical group 0.000 abstract 2
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- 125000000304 alkynyl group Chemical group 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical group 0.000 abstract 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 150000002431 hydrogen Chemical group 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- KIWSYRHAAPLJFJ-DNZSEPECSA-N n-[(e,2z)-4-ethyl-2-hydroxyimino-5-nitrohex-3-enyl]pyridine-3-carboxamide Chemical compound [O-][N+](=O)C(C)C(/CC)=C/C(=N/O)/CNC(=O)C1=CC=CN=C1 KIWSYRHAAPLJFJ-DNZSEPECSA-N 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 description 156
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- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- C07D213/73—Unsubstituted amino or imino radicals
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- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
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- C07D211/72—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
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Abstract
Un compuesto de fórmula**Fórmula** en la que: R1 está seleccionado entre arilo C6-12, y hetero arilo de 5-12 miembros, y cada hidrógeno en R' está opcionalmente sustituido con uno o más grupos R3; R3 es halógeno, alquilo C1-12, alquenilo C2-12, alquinilo C2-12, cicloalquilo C3-12, arilo C6-12, heteroalicíclico de 3-12 miembros, heteroarilo de 5-12 miembros, -S(O)mR4, -SO2NR4R5, -S(O)2OR4, -NO2, -NR4R5, - (CR6R7)nOR4, -CN, -C(O)R4, -OC(O)R4, -O(CR6R7)nR4, -NR4C(O)R5, -(CR6R7)nC(O)OR4, -C(>=NR6)NR4R5, -NR4C(O)NR5R6, -NR4S(O)pR5 o -C(O)NR4R5; cada R4, R5, R6 y R7 es independientemente hidrógeno, halógeno, alquilo C1-12, alquenilo C2-12, alquinilo C2- 12, cicloalquilo C3-12, arilo C6-12, heteroalicíclico de 3-12 miembros o heteroarilo de 5-12 miembros; cada R9 y R10 es independientemente hidrógeno o alquilo C1-12; A2 es arilo C6-12, o heteroarilo de 5-12 miembros, y A2 está opcionalmente sustituido con uno o más grupos R3; m es 0, 1 o 2; n es 0, 1, 2, 3 o 4; y p es 1 o 2; o una sal, solvato o hidrato farmacéuticamente aceptable del mismo.A compound of formula ** Formula ** in which: R1 is selected from C6-12 aryl, and 5-12 membered hetero aryl, and each hydrogen in R 'is optionally substituted with one or more R3 groups; R3 is halogen, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C3-12 cycloalkyl, C6-12 aryl, 3-12 membered heteroalicyclic, 5-12 membered heteroaryl, -S (O) mR4, -SO2NR4R5, -S (O) 2OR4, -NO2, -NR4R5, - (CR6R7) nOR4, -CN, -C (O) R4, -OC (O) R4, -O (CR6R7) nR4, -NR4C (O ) R5, - (CR6R7) nC (O) OR4, -C (> = NR6) NR4R5, -NR4C (O) NR5R6, -NR4S (O) pR5 or -C (O) NR4R5; each R4, R5, R6 and R7 is independently hydrogen, halogen, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C3-12 cycloalkyl, C6-12 aryl, 3-12 membered heteroalicyclic or 5-12 heteroaryl 12 members; each R9 and R10 is independently hydrogen or C1-12 alkyl; A2 is C6-12 aryl, or 5-12 membered heteroaryl, and A2 is optionally substituted with one or more R3 groups; m is 0, 1 or 2; n is 0, 1, 2, 3 or 4; and p is 1 or 2; or a pharmaceutically acceptable salt, solvate or hydrate thereof.
Description
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(continuación) (continuation)
- Sección B: Ejemplos L–17 a L–32 Section B: Examples L – 17 to L – 32
- imagen252 image252
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imagen253image253 imagen254image254 imagen255image255
- % de inhibición = 86 % inhibition = 86
- % de inhibición = 64 % de inhibición = 72 % de inhibición = 71 % inhibition = 64 % inhibition = 72 % inhibition = 71
- imagen256 image256
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imagen257image257 imagen258image258 imagen259image259
- % de inhibición = 77 % inhibition = 77
- % de inhibición = 2 % de inhibición = 74 % de inhibición = 64 % inhibition = 2 % inhibition = 74 % inhibition = 64
- imagen260 image260
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imagen261image261 imagen262image262
- % de inhibición = 86 % inhibition = 86
- % de inhibición = 80 % de inhibición = 85 % de inhibición = 92 % inhibition = 80 % inhibition = 85 % inhibition = 92
- Sección C: Ejemplos L–33 a L–48 Section C: Examples L – 33 to L – 48
- imagen263 image263
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imagen264image264
- % de inhibición = 63 % inhibition = 63
- % de inhibición = 62 % de inhibición = 55 % de inhibición = 62 % inhibition = 62 % inhibition = 55 % inhibition = 62
- imagen265 image265
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imagen266image266 imagen267image267
- % de inhibición = 75 % inhibition = 75
- % de inhibición = 88 % de inhibición = 77 % de inhibición = 55 % inhibition = 88 % inhibition = 77 % inhibition = 55
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(continuación) (continuation)
- Sección J: Ejemplos L–145 a L–160 Section J: Examples L – 145 to L – 160
- imagen273 image273
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imagen274image274 imagen275image275 imagen276image276
- % de inhibición = 70 % inhibition = 70
- % de inhibición = 81 % de inhibición = 58 % de inhibición = 53 % inhibition = 81 % inhibition = 58 % inhibition = 53
- imagen277 image277
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imagen278image278 imagen279image279 imagen280image280
- % de inhibición = 95 % inhibition = 95
- % de inhibición = 77 % de inhibición = 66 % de inhibición = 73 % inhibition = 77 % inhibition = 66 % inhibition = 73
- imagen281 image281
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imagen282image282 imagen283image283
- % de inhibición = 77 % inhibition = 77
- % de inhibición = 63 % de inhibición = 78 % de inhibición = 59 % inhibition = 63 % inhibition = 78 % inhibition = 59
- Sección K: Ejemplos L–161 a L–176 Section K: Examples L – 161 to L – 176
- imagen284 image284
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imagen285image285 imagen286image286
- % de inhibición = 79 % inhibition = 79
- % de inhibición = 66 % de inhibición = 83 % de inhibición = 61 % inhibition = 66 % inhibition = 83 % inhibition = 61
- imagen287 image287
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imagen288image288 imagen289image289
- % de inhibición = 88 % inhibition = 88
- % de inhibición = 67 % de inhibición = 66 % de inhibición = 90 % inhibition = 67 % inhibition = 66 % inhibition = 90
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Tabla 7 ––Table 7 ––
- Sección A: Ejemplos L–353 a L–368 Section A: Examples L – 353 to L – 368
- imagen302 image302
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imagen303image303 imagen304image304 imagen305image305
- % de inhibición = 24 % inhibition = 24
- % de inhibición = 19 % de inhibición = 32 % de inhibición = 22 % inhibition = 19 % inhibition = 32 % inhibition = 22
- imagen306 image306
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imagen307image307 imagen308image308 imagen309image309
- % de inhibición = 20 % inhibition = 20
- % de inhibición = 14 % de inhibición = 24 % de inhibición = 10 % inhibition = 14 % inhibition = 24 % inhibition = 10
- imagen310 image310
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imagen311image311 imagen312image312 imagen313image313
- % de inhibición = 8 % inhibition = 8
- % de inhibición = 37 % de inhibición = 36 % de inhibición = 6 % inhibition = 37 % inhibition = 36 % inhibition = 6
- imagen314 image314
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imagen315image315 imagen316image316 imagen317image317
- % de inhibición = 8 % inhibition = 8
- % de inhibición = 9 % de inhibición = 6 % de inhibición = 27 % inhibition = 9 % inhibition = 6 % inhibition = 27
- Sección B: Ejemplos L–369 a L–384 Section B: Examples L – 369 to L – 384
- imagen318 image318
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imagen319image319 imagen320image320 imagen321image321
- % de inhibición = 10 % inhibition = 10
- % de inhibición = 19 % de inhibición = 10 % de inhibición = 49 % inhibition = 19 % inhibition = 10 % inhibition = 49
- imagen322 image322
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imagen323image323 imagen324image324
- % de inhibición = 19 % inhibition = 19
- % de inhibición = 5 % de inhibición = 10 % de inhibición = 10 % inhibition = 5 % inhibition = 10 % inhibition = 10
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(continuación) (continuation)
- Sección D: Ejemplos L–401 a L–416 Section D: Examples L – 401 to L – 416
- imagen326 image326
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imagen327image327 imagen328image328
- % de inhibición = 9 % inhibition = 9
- % de inhibición = 11 % de inhibición = 4 % de inhibición = 41 % inhibition = 11 % inhibition = 4 % inhibition = 41
- imagen329 image329
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imagen330image330 imagen331image331
- % de inhibición = 21 % inhibition = 21
- % de inhibición = 14 % de inhibición = 13 % de inhibición = 12 % inhibition = 14 % inhibition = 13 % inhibition = 12
- imagen332 image332
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imagen333image333 imagen334image334
- % de inhibición = 31 % inhibition = 31
- % de inhibición = 19 % de inhibición = 27 % de inhibición = 25 % inhibition = 19 % inhibition = 27 % inhibition = 25
- imagen335 image335
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imagen336image336 imagen337image337
- % de inhibición = 31 % inhibition = 31
- % de inhibición = 45 % de inhibición = 11 % de inhibición = 77 % inhibition = 45 % inhibition = 11 % inhibition = 77
- Sección E: Ejemplos L–417 a L–432 Section E: Examples L – 417 to L – 432
- imagen338 image338
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imagen339image339 imagen340image340
- % de inhibición = 11 % inhibition = 11
- % de inhibición = 9 % de inhibición = 12 % de inhibición = 7 % inhibition = 9 % inhibition = 12 % inhibition = 7
- imagen341 image341
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imagen342image342 imagen343image343
- % de inhibición = 10 % inhibition = 10
- % de inhibición = 14 % de inhibición = 10 % de inhibición = 12 % inhibition = 14 % inhibition = 10 % inhibition = 12
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(continuación) (continuation)
- Sección H: Ejemplos L–465 a L–480 Section H: Examples L – 465 to L – 480
- imagen346 image346
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imagen347image347 imagen348image348 imagen349image349
- % de inhibición = 14 % inhibition = 14
- % de inhibición = 18 % de inhibición = 13 % de inhibición = 13 % inhibition = 18 % inhibition = 13 % inhibition = 13
- imagen350 image350
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imagen351image351 imagen352image352 imagen353image353
- % de inhibición = 10 % inhibition = 10
- % de inhibición = 9 % de inhibición = 10 % de inhibición = 9 % inhibition = 9 % inhibition = 10 % inhibition = 9
- imagen354 image354
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imagen355image355 imagen356image356 imagen357image357
- % de inhibición = 50 % inhibition = 50
- % de inhibición = 39 % de inhibición = 51 % de inhibición = 27 % inhibition = 39 % inhibition = 51 % inhibition = 27
- imagen358 image358
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imagen359image359 imagen360image360 imagen361image361
- % de inhibición = 29 % inhibition = 29
- % de inhibición = 24 % de inhibición = 15 % de inhibición = 17 % inhibition = 24 % inhibition = 15 % inhibition = 17
- Sección I: Ejemplos L–481 a L–496 Section I: Examples L – 481 to L – 496
- imagen362 image362
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imagen363image363 imagen364image364 imagen365image365
- % de inhibición = 18 % inhibition = 18
- % de inhibición = 20 % de inhibición = 19 % de inhibición = 16 % inhibition = 20 % inhibition = 19 % inhibition = 16
- imagen366 image366
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imagen367image367 imagen368image368
- % de inhibición = 18 % inhibition = 18
- % de inhibición = 22 % de inhibición = 63 % de inhibición = 17 % inhibition = 22 % inhibition = 63 % inhibition = 17
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(continuación) (continuación) (continued) (continued)
- Sección K: Ejemplos L–513 a L–528 Section K: Examples L – 513 to L – 528
- imagen370 image370
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imagen371image371 imagen372image372 imagen373image373
- % de inhibición = 16 % inhibition = 16
- % de inhibición = 17 % de inhibición = 17 % inhibition = 17 % inhibition = 17
- % de inhibición = 16 % inhibition = 16
- imagen374 image374
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imagen375image375 imagen376image376 imagen377image377
- % de inhibición = 19 % inhibition = 19
- % de inhibición = 15 % de inhibición = 8 % de inhibición = 14 % inhibition = 15 % inhibition = 8 % inhibition = 14
- imagen378 image378
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imagen379image379
- % de inhibición = 23 % inhibition = 23
- % de inhibición = 7 % de inhibición = 9 % de inhibición = 5 % inhibition = 7 % inhibition = 9 % inhibition = 5
- imagen380 image380
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imagen381image381
- % de inhibición = 5 % inhibition = 5
- % de inhibición = 10 % de inhibición = 9 % de inhibición = 9 % inhibition = 10 % inhibition = 9 % inhibition = 9
- Sección L: Ejemplos L–529 a L–548 Section L: Examples L – 529 to L – 548
- imagen382 image382
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imagen383image383 imagen384image384
- % de inhibición = 9 % inhibition = 9
- % de inhibición = 8 % de inhibición = 8 % de inhibición = 27 % inhibition = 8 % inhibition = 8 % inhibition = 27
- imagen385 image385
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imagen386image386 imagen387image387
- % de inhibición = 12 % inhibition = 12
- % de inhibición = 18 % de inhibición = 4 % de inhibición = 10 % inhibition = 18 % inhibition = 4 % inhibition = 10
- Sección L: Ejemplos L–529 a L–548 Section L: Examples L – 529 to L – 548
- imagen388 image388
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imagen389image389 imagen390image390 imagen391image391
- % de inhibición = 12 % inhibition = 12
- % de inhibición = ‒2 % de inhibición = 28 % de inhibición = 11 % inhibition = ‒2 % inhibition = 28 % inhibition = 11
- imagen392 image392
-
imagen393image393 imagen394image394 imagen395image395
- % de inhibición = 5 % inhibition = 5
- % de inhibición = 6 % de inhibición = 7 % de inhibición = 6 % inhibition = 6 % inhibition = 7 % inhibition = 6
- imagen396 image396
-
imagen397image397 imagen398image398
- % de inhibición = 11 % inhibition = 11
- % de inhibición = 11 % inhibition = 11
- % de inhibición = 64 % de inhibición = 16 % inhibition = 64 % inhibition = 16
Tabla 8 Table 8
- Sección A: Ejemplos L–549 a L–561 Section A: Examples L – 549 to L – 561
- imagen399 image399
-
imagen400image400 imagen401image401
- % de inhibición = 11 % inhibition = 11
- % de inhibición = 13 % de inhibición = 11 % de inhibición = 20 % inhibition = 13 % inhibition = 11 % inhibition = 20
- imagen402 image402
-
imagen403image403 imagen404image404
- % de inhibición = 25 % inhibition = 25
- % de inhibición = 14 % de inhibición = 21 % de inhibición = 12 % inhibition = 14 % inhibition = 21 % inhibition = 12
––––
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